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维生素 E TPGS 在药物传递中的应用。

The applications of Vitamin E TPGS in drug delivery.

机构信息

Tongji School of Pharmacy, Huazhong University of Science and Technology, Wuhan 430030, PR China.

出版信息

Eur J Pharm Sci. 2013 May 13;49(2):175-86. doi: 10.1016/j.ejps.2013.02.006. Epub 2013 Feb 26.

Abstract

D-α-Tocopheryl polyethylene glycol 1000 succinate (simply TPGS or Vitamin E TPGS) is formed by the esterification of Vitamin E succinate with polyethylene glycol 1000. As novel nonionic surfactant, it exhibits amphipathic properties and can form stable micelles in aqueous vehicles at concentration as low as 0.02 wt%. It has been widely investigated for its emulsifying, dispersing, gelling, and solubilizing effects on poorly water-soluble drugs. It can also act as a P-glycoprotein (P-gp) inhibitor and has been served as an excipient for overcoming multidrug resistance (MDR) and for increasing the oral bioavailability of many anticancer drugs. Since TPGS has been approved by FDA as a safe pharmaceutic adjuvant, many TPGS-based drug delivery systems (DDS) have been developed. In this review, we discuss TPGS properties as a P-gp inhibitor, solubilizer/absorption and permeation enhancer in drug delivery and TPGS-related formulations such as nanocrystals, nanosuspensions, tablets/solid dispersions, adjuvant in vaccine systems, nutrition supplement, plasticizer of film, anticancer reagent and so on. This review will greatly impact and bring out new insights in the use of TPGS in DDS.

摘要

D-α-生育酚聚乙二醇 1000 琥珀酸酯(简称 TPGS 或维生素 E TPGS)是由琥珀酸维生素 E 与聚乙二醇 1000 酯化而成。作为一种新型的非离子表面活性剂,它具有两亲性,可以在低至 0.02wt%的浓度下在水相载体中形成稳定的胶束。它已广泛研究其对亲脂性差的药物的乳化、分散、胶凝和增溶作用。它还可以作为 P 糖蛋白(P-gp)抑制剂,并已作为克服多药耐药性(MDR)和提高许多抗癌药物口服生物利用度的赋形剂。由于 TPGS 已被 FDA 批准为安全的药物辅料,因此已经开发了许多基于 TPGS 的药物递送系统(DDS)。在这篇综述中,我们讨论了 TPGS 作为 P-gp 抑制剂、增溶剂/吸收促进剂和渗透增强剂在药物递送中的性质,以及与 TPGS 相关的制剂,如纳米晶体、纳米混悬剂、片剂/固体分散体、疫苗系统中的佐剂、营养补充剂、膜的增塑剂、抗癌试剂等。这篇综述将对 TPGS 在 DDS 中的应用产生重大影响,并带来新的见解。

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